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Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Inflammatory and Anti-Allergy Agents) (v.10, #3)
Editorial [Hot-Topic: Optimizing a Therapeutic With Anti-Inflammatory Agents:Novel Drug Delivery Systems (Guest Editor: Carla Martins Lopes)] by Carla Martins Lopes (pp. 153-153).
In the early 1900s, a German scientist developed the concept of “magic bullet”. This concept means targeting diseasedtissues directly with the drug. Nowadays, medicinal scientists continue to search for the magic bullet suitable for the treatmentof the major health threats including pain and inflammatory diseases. Efficient drug delivery systems are as important as drugthemselves.Anti-inflammatory therapeutic agents are among the most commonly prescribed drugs worldwide. Nonetheless, thetreatment with anti-inflammatory agents is often associated with important problems such as delivery of drug to the appropriatesite of action and adverse gastrointestinal tract effects. Therefore, alternative approaches to target therapeutic concentrations ofanti-inflammatory agents are required. Over the last decades, the optimization of drug therapy by means of delivery systems design had attracted the attention ofmany researchers. Drug delivery systems can provide multiple advantages to existing drugs as well as new drugs. Noveleffective delivery systems that potentially optimize dosage, enhancing the drug performance and minimize systemic side effectscompared to current methods of dosing drugs may be a better investment and more effective for patients than creating a newdrug. The type of drug to be formulated will define the type of release to achieve. The purpose of the current special issue is to compile the recent literature advances in optimizing and enhancing of antiinflammatorytherapy with special focus to the state of the art on novel drug delivery approaches (e.g. modulated and targeteddrug release). Concerning this aim, in the eight papers of the present special issue, it will discuss several topics, namelydifferent administrations routes of anti-inflammatory agents and several pharmaceutical systems and carriers.As guest editor, I would like to thank all the authors of this special issue for contributing high quality papers. I would alsowish to thank all the referees (two per paper) who have critically evaluated the articles within the stipulated time: LoredanaSerpe, Amelia Avachat, Mihaela Trif, Carla M. Lopes, Mª del Carmen Lozano Estevan, Mark Saunders, Jayachandra Babu,Joao Jose Sousa, Gary Moss, Zhiyong Qian, K. S. Rathore, Evren Gokce, Gabriele Nicolini, Amrita Bajaj, Averineni RanjithKumar and Kok Khiang Peh. Finally, I would like to thank Editor-in-Chief, Professor Bahar Tunctan, for giving us the greatopportunity of organizing this special issue.
Pharmaceutical Approaches for Optimizing Oral Anti-Inflammatory Delivery Systems by Lopes C.M., Oliveira R., Silva A.C. (pp. 154-165).
The purpose of the present review is to compile the recent literature in the field of anti-inflammatorytreatments, with special focus to the state-of-the-art on pharmaceutical approaches for optimizing oral administration.Attending to the drawbacks associated with the use of these types of drugs, the development of oral modulated releaseformulations is highly desirable in order to achieve improved therapeutic efficacy and patient compliance. Severaltechnological systems and their advantages in modulated and targeted drug releases (gastroretention or colonic release)have been described: matrix systems, coated dosage forms, osmotic pressure based formulations, prodrugs, colloidalcarriers, microparticles and other carriers. These new approaches seem to be promising and have been considered bypharmaceutical companies.
Novel Carriers for Controlled Site Specific Delivery of Anti-Inflammatory Agents by Virendra Gajbhiye, N.K. Jain (pp. 166-179).
Acute and chronic inflammation associated with pain may result in diseases and disorders such as hay fever,atherosclerosis, discrepancy in blood pressure, mental despair, and personality disorganization, if it is not given treatmentat the beginning itself. Most anti-inflammatory drugs employed for pain relief intention for long term display extensiveadverse reports such as creating renal side effects, gastrointestinal side effects, gastrointestinal bleeding, perforation etc.and few further side effects such as hypersensitivity reactions and distinct salicylate intoxication. Targeting drugs to theinflamed region, in the treatment of rheumatoid arthritis, osteo-arthritis, inflammatory bowel disease and other chronicmusculoskeletal conditions would reduce the amount of drug required to control the disease, with possible additionalreduction or even elimination of adverse side effects. Novel drug carrier systems are playing an important role in targetinganti-inflammatory drugs to inflamed region. Carriers like liposomes, microspheres, nanoparticles and dendrimer, etc. haveshown potential to supplement sustained drug delivery, extended duration of action with improved patient compliance.This review focuses on the current state of the art in the field of nanocarrier mediated controlled and site specific deliveryof anti-inflammatory drugs.
Chronopharmaceutical Delivery of Anti-Inflammatory Drugs by Baratta P., Lopes C.M. (pp. 180-189).
The human body follows 24 hours cycles called the circadian rhythm that affect many physiological andphysiopathological processes. Chronotherapeutic diseases include asthma, cardiovascular diseases, cancer, rheumatoidarthritis and other algesia processes. Drugs behaviours in the human body are also strongly affected by circadian changes,especially in what concerns absorption and elimination. Anti-inflammatory drugs are excellent candidates tochronotherapeutical delivery. Chronotherapeutic products are able to synchronize drug delivery with circadian rhythms inorder to enhance efficacy and reduce side effects. These products mainly offer pulsatile release that follow a sigmoidrelease profile with a combination of periods of lag time and periods of fast drug release. Many technologies, either singleunits or multiparticulate systems, have been suggested and some have been successfully marketed improving patientsadherence and quality of life. This review aims to describe the circadian rhythms and their influences in therapeutics aswell as the technologies that have been proposed to develop chronopharmaceutical dosage forms.
Mucoadhesive Buccal Systems as a Novel Strategy for Anti-Inflammatory Drugs Administration by Ana Figueiras, Amelia Vieira, Susana Simoes, Francisco Veiga (pp. 190-202).
This is a review article that intends to emphasize the advantages of buccal delivery as an alternative route ofadministration of anti-inflammatory drugs. The oral cavity has a number of features that make it desirable for drugadministration: a rich blood supply that drains directly into the jugular vein, thus bypassing the liver and sparing the drugfrom first pass metabolism. To understand this point of view, some considerations are done relatively to the oral mucosalstructural characteristics with relevance to drug administration, oral mucosal permeability, as well as drug absorptionmechanisms through oral cavity. However, to design a buccal delivery system, it is necessary to take in account theresidence time of drug formulation in the buccal mucosa. Mucoadhesion mechanism can be a solution to overcome thislimitation. For this reason the main buccoadhesive pharmaceutical forms are approached, as well as the importance of oralmucosal in buccal anti-inflammatory drug delivery systems in terms of future perspectives.
Drug Delivery Systems for Ophthalmic Administration of Antiinflammatory Agents by Yolanda Diebold, Laura Contreras-Ruiz, Isabel Arranz-Valsero, Laura Garcia-Posadas (pp. 203-214).
Anti-inflammatory agents are routinely used to treat inflammatory diseases affecting both anterior and/orposterior segments of the eye. Corticosteroids and NSAIDs can be administered either topically onto the ocular surfacestructures or injected into the eye. However, one of the most important handicaps of ocular treatments is the presence ofseveral anatomical and physiological barriers in the eye that drastically reduce drug access to the target site. Thehydrophobicity of anti-inflammatory agents, low drug bioavailability, and the invasiveness of intraocular drug deliveryare main reasons to explore the potential application of drug delivery-related technologies to develop new antiinflammatoryocular therapies. This review summarizes conventional anti-inflammatory treatments for ocular diseases andthe ongoing research efforts to develop improved drug delivery systems. Micro-size intraocular implants, microparticles,nanoparticles, and liposomes are the preferred delivery systems in study.
Pulmonary and Nasal Anti-Inflammatory and Anti-Allergy Inhalation Aerosol Delivery Systems by Xiao Wu, Oreoluwa O. Adedoyin, Heidi M. Mansour (pp. 215-229).
Most respiratory infections, diseases and allergic reactions have varying degrees of inflammation.Inflammation is a natural immunodefensive response to the presence of allergens or foreign particles that come intocontact or affect the cells and tissues within the respiratory tract. The three main types of therapeutic drug classesavailable for anti-inflammatory and anti-allergy effects are corticosteroids, antihistamines and decongestants.Corticosteroid drugs for pulmonary inhalation and/or nasal delivery include beclomethasone dipropionate, budesonide,ciclesonide, fluticasone furoate, fluticasone propionate, mometasone furoate, and triamcinolone acetonide. Antihistaminedrugs for nasal delivery include azelastine and olopatadine. Two common decongestants available are oxymetazoline andphenylephrine. Another therapeutic class, the anticholinergic agents, such as ipratropium bromide and tiotropiumbromide, are used in pulmonary delivery in the treatment of inflammatory diseases such as asthma and chronic obstructivepulmonary disease. The mast cell stabilizer therapeutic class, cromolyn sodium, can be used to prevent and relieve nasalallergic symptoms. Additionally cromolyn sodium was the first dry powder inhaler product for pulmonary drug deliveryseveral decades ago and currently is on the market as a pressurized metered dose inhaler for pulmonary inhalationdelivery. Based on the devices used in pulmonary drug delivery, this route can be subdivided into three categories; namelynebulizers, pressurized metered dose inhalers, and dry powder inhalers. Nasal delivery of anti-inflammatory and antiallergydrugs is most commonly available commercially in an aqueous spray form. This article comprehensively reviewsand discusses different kinds of drugs used for anti-inflammatory and anti-allergic effects via the pulmonary and nasaldelivery route, as well as their mechanisms of action, marketed products, disease state indications while highlighting drugdelivery and therapeutic aspects.
Cyclodextrin-Based Carriers for Topical Delivery of Anti-Inflammatory Agents by Rita Oliveira, Pedro Coelho (pp. 230-239).
Anti-inflammatory agents topically applied are appropriate in the treatment of skin diseases, restricting thetherapeutical action to the affected area and reducing systemic side effects. On the other hand, systemic activity is the aimof transdermal delivery, which can be used to minimize the first pass metabolism but also to control systemic side effects,e.g., nonsteroidal anti-inflammatory drugs. The main limitation of this route is to overcome the stratum corneum, the outermost skin barrier. In order to achievetherapeutic concentrations and to improve the drug flux, permeation enhancers are used to optimize drug permeationthrough the skin. Cyclodextrins and their derivatives are capable of forming inclusion complexes with poor water soluble drugs improvingtheir water solubility, bioavailability and stability, among other features. Cyclodextrins have been used as permeationenhancers although their mechanism it not yet well known. They can also be useful in the design of new drug carriers forskin delivery, by increasing the solubility of drugs hence providing high drug content systems. Improving the drugstability and promoting drug permeation are also desirable properties that cyclodextrins can provide to novel drug carriers.Several anti-inflammatory drugs have been incorporated into various skin delivery cyclodextrin-based systems such asliposomes, solid lipid nanoparticles and microemulsions.
In Vitro Evaluation of Bioadhesive Films Containing Ibuprofen by C. Padula, S. Nicoli, P. Santi (pp. 240-245).
The aim of this work was to develop films containing ibuprofen and to study their in vitro permeationcharacteristics across pig ear skin, a valid model for human skin. Films containing 5% (w/w) of ibuprofen were preparedand tested: the effect of the chemical enhancers polyvynil pyrrolidone, propylene glycol, menthol and 2-pyrrolidone wasevaluated as well. From the data obtained it can be concluded that the bioadhesive film formulated can act as adermal/transdermal delivery system for the administration of ibuprofen. The film is easy to handle before the applicationand then it adapts to skin irregularities increasing the effective contact area. The permeation kinetic across the skin wasnot linear, suggesting that the film acts as a matrix controlling drug delivery. The introduction of chemical enhancers inthe formulation or the application of the film in the presence of menthol did not modify the permeation of ibuprofenacross pig ear skin. On the other hand the application of an occlusive layer increased the amount of ibuprofen permeatedfrom the film and the permeation profile obtained was comparable to that obtained from the commercial formulationapplied in finite dose conditions.